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DE60006665D1 - C17-ALKYL SUBSTITUTED STEROID COMPOUNDS WITH AN AROMATIC A-RING FOR THERAPEUTIC USE - Google Patents

C17-ALKYL SUBSTITUTED STEROID COMPOUNDS WITH AN AROMATIC A-RING FOR THERAPEUTIC USE

Info

Publication number
DE60006665D1
DE60006665D1 DE60006665T DE60006665T DE60006665D1 DE 60006665 D1 DE60006665 D1 DE 60006665D1 DE 60006665 T DE60006665 T DE 60006665T DE 60006665 T DE60006665 T DE 60006665T DE 60006665 D1 DE60006665 D1 DE 60006665D1
Authority
DE
Germany
Prior art keywords
sup
group
hydrogen atom
hydroxyl
aromatic
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Fee Related
Application number
DE60006665T
Other languages
German (de)
Other versions
DE60006665T2 (en
Inventor
Henry Hesse
Katugam Setty
Malathi Ramgopal
Sanga Kugabalusooriar
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Research Institute for Medicine and Chemistry Inc
Original Assignee
Research Institute for Medicine and Chemistry Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Research Institute for Medicine and Chemistry Inc filed Critical Research Institute for Medicine and Chemistry Inc
Publication of DE60006665D1 publication Critical patent/DE60006665D1/en
Application granted granted Critical
Publication of DE60006665T2 publication Critical patent/DE60006665T2/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0072Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the A ring of the steroid being aromatic
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18Feminine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/02Drugs for disorders of the endocrine system of the hypothalamic hormones, e.g. TRH, GnRH, CRH, GRH, somatostatin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/18Drugs for disorders of the endocrine system of the parathyroid hormones
    • A61P5/20Drugs for disorders of the endocrine system of the parathyroid hormones for decreasing, blocking or antagonising the activity of PTH
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Neurosurgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Pregnancy & Childbirth (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Steroid Compounds (AREA)

Abstract

Formula (I) in which: R<SUP>1 </SUP>and R<SUP>2</SUP>, which may be the same or different, each represents a lower alkyl, alkenyl or alkynyl group; R<SUP>3 </SUP>represents a methyl group having alpha- or beta-configuration; R<SUP>4 </SUP>represents a hydrogen atom or an etherifying or esterifying group; R<SUP>5 </SUP>represents a hydrogen atom, a hydroxyl group or a lower alkoxy group; X represents a group OR<SUP>4</SUP>, or a group NR<SUP>6</SUP>R<SUP>7 </SUP>wherein R<SUP>6 </SUP>represents a hydrogen atom, an aliphatic or araliphatic group, or an acyl group comprising an aliphatic, araliphatic or aryl group linked to the nitrogen atom by way of a carbonyl group; and R<SUP>7 </SUP>is a hydrogen atom or a lower alkyl group; Y represents a lower alkylene, alkenylene or alkynylene group optionally substituted by a hydroxyl, etherified hydroxyl or esterified hydroxyl group; exhibit potent effects on modulation of cell growth and differentiation, while having low calcaemic activity.
DE60006665T 1999-05-11 2000-05-11 C17-ALKYL SUBSTITUTED STEROID COMPOUNDS WITH AN AROMATIC A-RING FOR THERAPEUTIC USE Expired - Fee Related DE60006665T2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9910934.0A GB9910934D0 (en) 1999-05-11 1999-05-11 Chemical compounds
PCT/GB2000/001813 WO2000068246A1 (en) 1999-05-11 2000-05-11 Steroid compounds with a c17-alkyl side chain and an aromatic a-ring for use in therapy

Publications (2)

Publication Number Publication Date
DE60006665D1 true DE60006665D1 (en) 2003-12-24
DE60006665T2 DE60006665T2 (en) 2004-10-07

Family

ID=10853250

Family Applications (1)

Application Number Title Priority Date Filing Date
DE60006665T Expired - Fee Related DE60006665T2 (en) 1999-05-11 2000-05-11 C17-ALKYL SUBSTITUTED STEROID COMPOUNDS WITH AN AROMATIC A-RING FOR THERAPEUTIC USE

Country Status (21)

Country Link
US (2) US6881730B1 (en)
EP (1) EP1179005B1 (en)
JP (1) JP2002544137A (en)
KR (1) KR100690040B1 (en)
CN (1) CN1158297C (en)
AT (1) ATE254629T1 (en)
AU (1) AU779743B2 (en)
CA (1) CA2373443A1 (en)
CZ (1) CZ297316B6 (en)
DE (1) DE60006665T2 (en)
DK (1) DK1179005T3 (en)
ES (1) ES2207509T3 (en)
GB (1) GB9910934D0 (en)
HK (1) HK1046001B (en)
HU (1) HUP0201047A3 (en)
IL (2) IL146442A0 (en)
NO (1) NO319949B1 (en)
NZ (1) NZ515482A (en)
PT (1) PT1179005E (en)
WO (1) WO2000068246A1 (en)
ZA (1) ZA200109272B (en)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6908910B2 (en) 1993-08-06 2005-06-21 The Children's Medical Center Corporation Estrogenic compounds as anti-mitotic agents
GB9910934D0 (en) * 1999-05-11 1999-07-14 Res Inst Medicine Chem Chemical compounds
US7087592B1 (en) 1999-08-23 2006-08-08 Entre Med, Inc. Compositions comprising purified 2-methoxyestradiol and methods of producing same
NZ523042A (en) * 2000-05-11 2004-05-28 Res Inst Medicine Chem 2-substituted pregna-1, 3, 5 (10) -triene and chola-1, 3, 5 (10)-triene derivatives and their biological activity
US6995278B2 (en) 2000-08-18 2006-02-07 Entre Med, Inc. Antiangiogenic agents
US7135581B2 (en) 2000-08-18 2006-11-14 Entremed, Inc. Antiangiogenic agents
JP2004537499A (en) * 2000-11-27 2004-12-16 エントレメッド インコーポレイテッド Anti-angiogenic drugs
WO2002092100A1 (en) * 2001-05-11 2002-11-21 Marsden, John, Christopher 17-(c(ch3) (ch2) o-3c (r4, r5) n (r6, r7))-substituted 19-nor-pregna-1, 3, 5(10)-triene derivatives and their medical use
AU2004275693A1 (en) 2003-05-28 2005-04-07 Entremed, Inc. Antiangiogenic agents
JP2007529426A (en) 2004-03-12 2007-10-25 エントレメッド インコーポレイテッド Anti-angiogenic drugs
CA2646065C (en) 2006-03-20 2014-01-14 Entremed, Inc. Disease modifying anti-arthritic activity of 2-methoxyestradiol
NZ581081A (en) * 2007-06-19 2012-12-21 Kythera Biopharmaceuticals Inc Synthetic deoxycholic acid (dca) or an ester, hydroxamale, or hydroxyamide thereof
US8242294B2 (en) 2007-06-19 2012-08-14 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
JOP20180077A1 (en) 2007-06-19 2019-01-30 Kythera Biopharmaceuticals Inc Synthetic bile acid compositions and methods
US20080318870A1 (en) 2007-06-19 2008-12-25 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
WO2013036835A1 (en) * 2011-09-08 2013-03-14 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
RS67266B1 (en) 2013-03-13 2025-10-31 Sage Therapeutics Inc Neuroactive steriods and methods of use thereof
WO2015195967A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
BR112018000129B1 (en) 2015-07-06 2024-01-09 Sage Therapeutics, Inc Oxysterol compounds, their uses and pharmaceutical composition
SMT202100476T1 (en) 2015-07-06 2021-09-14 Sage Therapeutics Inc Oxysterols and methods of use thereof
JP6882996B2 (en) 2015-07-06 2021-06-02 セージ セラピューティクス, インコーポレイテッド Oxysterols and how to use them
SI3436022T1 (en) 2016-04-01 2022-08-31 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
ES2884071T3 (en) 2016-07-07 2021-12-10 Sage Therapeutics Inc 11-substituted 24-hydroxysteroles for the treatment of NMDA-related conditions
MX392270B (en) 2016-09-30 2025-03-24 Sage Therapeutics Inc C7-SUBSTITUTED OXYSTEROLS AND METHODS OF USING THEM.
EP4105223B1 (en) 2016-10-18 2025-04-30 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
CN110267966B (en) 2016-10-18 2022-07-08 萨奇治疗股份有限公司 Oxysterols and methods of using the same
CN115040524A (en) * 2022-07-27 2022-09-13 深圳市中西医结合医院 Use of 4-cholesten-3-ones for the treatment of multiple myeloma bone disease

Family Cites Families (6)

* Cited by examiner, † Cited by third party
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US3562260A (en) * 1965-08-23 1971-02-09 Ormonoterapia Richter Spa 2-carbonyl-estratrienes and method of their preparation
GB1267915A (en) * 1968-05-24 1972-03-22 Glaxo Lab Ltd Ring a-substituted ring a-aromatic steroids
FR2528434B1 (en) * 1982-06-11 1985-07-19 Roussel Uclaf NOVEL 19-NOR STEROIDS SUBSTITUTED IN 11B AND POSSIBLY IN 2, THEIR PREPARATION PROCESS AND THEIR APPLICATION AS A MEDICAMENT
JP2623285B2 (en) * 1988-03-09 1997-06-25 雪印乳業株式会社 Method for producing 2 (3-hydroxy-1,3,5 (10) -estrien-17-yl) propionic acid
GB9910934D0 (en) * 1999-05-11 1999-07-14 Res Inst Medicine Chem Chemical compounds
US6967195B2 (en) * 2000-05-11 2005-11-22 Research Institute For Medicine And Chemistry, Inc. 2-substituted pregna-1-3,5(10) triene and chola-1,3,5(10) triene derivatives and their biological activity

Also Published As

Publication number Publication date
AU779743B2 (en) 2005-02-10
NZ515482A (en) 2004-05-28
JP2002544137A (en) 2002-12-24
EP1179005B1 (en) 2003-11-19
HK1046001B (en) 2004-12-24
US6881730B1 (en) 2005-04-19
DE60006665T2 (en) 2004-10-07
NO20015520D0 (en) 2001-11-12
NO319949B1 (en) 2005-10-03
CN1158297C (en) 2004-07-21
IL146442A0 (en) 2002-07-25
US20050171075A1 (en) 2005-08-04
AU4596000A (en) 2000-11-21
HK1046001A1 (en) 2002-12-20
ZA200109272B (en) 2003-02-26
GB9910934D0 (en) 1999-07-14
EP1179005A1 (en) 2002-02-13
KR20020013542A (en) 2002-02-20
HUP0201047A3 (en) 2003-07-28
KR100690040B1 (en) 2007-03-09
CZ20014049A3 (en) 2002-04-17
IL146442A (en) 2006-10-05
CZ297316B6 (en) 2006-11-15
CA2373443A1 (en) 2000-11-16
PT1179005E (en) 2004-04-30
WO2000068246A1 (en) 2000-11-16
CN1358193A (en) 2002-07-10
HUP0201047A2 (en) 2002-08-28
ES2207509T3 (en) 2004-06-01
ATE254629T1 (en) 2003-12-15
DK1179005T3 (en) 2004-03-01
NO20015520L (en) 2002-01-09

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